Hays first reported on the topical application of glycopyrrolate for facial sweating associated with eating (gustatory sweating). (1, 2) Subsequently others have reported on the use of topical glycopyrrolate for hyperhidrosis and gustatory sweating. Oral glycopyrrolate has also been used for hyperhidrosis. Glycopyrrolate does not cure any underlying causes of hyperhidrosis or gustatory sweating, but reduces or prevents the resulting excessive sweating.
Use of glycopyrrolate as an anti-secretagogue in the treatment of peptic ulcer disease commenced in Canada in 1961. It continues to be used as an antisialogogue in patients with drooling and as a premedication for anaesthesia to prevent excessive secretions.
Glycopyrrolate is a quaternary amine, which acts as an antimuscarinic, anticholinergic agent. It does not cross the blood brain barrier and it penetrates biological membranes slowly and therefore, when given topically leads to very few side effects.
As with all members of this class, glycopyrrolate should not be used by people with glaucoma or cardiac arrhythmias. Glycopyrrolate should also not be used by people with bladder obstruction, a rapid heart rate, an allergy to glycopyrrolate, or when pregnant or breast-feeding.
For most people sweating is a normal response to heat stress and is important in maintaining body temperature. However, in some individuals sweating can be excessive and unrelated to heat stress. This excessive sweating can be embarrassing and can severely limit social activities. The areas typically involved in excessive perspiration are 1) face including the neck and scalp 2) armpits 3) hands 4) back of the knees 5) feet 6) groin, and 7) in the case of compensatory sweating, the trunk.
Nerve impulses from the brain stimulate sweat glands and cause perspiration. Sometimes the nerves stimulate excessive sweating unrelated to the normal process of temperature control.
The use of topical glycopyrrolate has been reported over the past 20 years. Here is a table of clinical papers reporting use of glycopyrrolate and the topical formulation used.
Treatment of Hyperhidrosis and Gustatory SweatingAuthorYearConcentrationFormulationNotesHay19780.5 & 1.0%Solution and creamCotton applicator used to applypresentationssolution.Hay19820.5, 1 & 2%Roll-on solution,Glycopyrrolate crystalized outdistilled water used.when concentrations above 2%.pH adjusted to 2.5 to 4.0 Fewpatients need to rub lotion into theskin to get better effects.Hay19822 & 4%HEB cream baseSolution worked better than(Barnes-Hindcream.May19890.5, & 2.0%0.5 & 2.0% roll-on;almost all patients obtained total2.0% cream. Used Haysor partial relief. Placeboformulation.treatment yielded no response.Atkin19960.50%cetamacrogol ACrushed Robinul ™ tablets mixedformulation cream baseinto creamShaw19970.50%cetamacrogol Aformulation cream baseSeukeran1998  2%cetamacrogol ACould not get cream into hairline.formulation cream baseCream and sweat mixtureunacceptable.Seukeran19980.50%aqueous solutionWorked wellUrman19990.50%Lotion in a roll-ondispenser
Here are the details from one of these papers. In a recent clinical trial (Shaw, J. E., C. A. Abbott, et al. (1997)) to determine if topical glycopyrrolate is able to control diabetic gustatory sweating, the authors found that topical glycopyrrolate is an acceptable safe and effective treatment for diabetic gustatory sweating. A placebo or glycopyrrolate 0.5% cream was self administered by hand to the face and neck. A challenge test was administered, at baseline and at the end of each of the treatment periods. The sweat challenge test measures the amount of sweat produced on the forehead relative to reference sites on the arm and the leg. Glycopyrrolate treated patients had a statistically significant reduction in sweat production during the challenge test (p=0.008). Daily diary records indicated that topical glycopyrrolate treatment resulted in a reduction in frequency and severity of gustatory sweating compared to the placebo treatment (p=0.004). One patient out of 14 discontinued therapy because of a local skin reaction. No other adverse effects were reported.